The phytochemical constituents, antioxidant capabilities and enzyme inhibitory potentials of aqueous extract of Vitex simplicifolia leaf were investigated. The plant was assessed for its phytochemical availability using GC-FID; antioxidant activity was assessed while lactate dehydrogenase (LDH) inhibitory potential was analyzed by chemical method. The result revealed the presence of phytochemicals in which Anthocyanin (Flavonoid) showed the highest significant (p≤0.05) increase in concentration when compared to other secondary metabolites.